Pharmacodynamics and pharmacokinetics
Acetylsalicylic acid - what is it?
Acetylsalicylic acid is Aspirin , a salicylic ester of acetic (ethanoic) acid.
The formula of acetylsalicylic acid is (ASA) - C₉H₈O₄.
OKPD code 24.42.13.142 ( acetylsalicylic acid mixed with other drugs).
Receiving ASA
In the production of ASA, the method of esterification of salicylic acid with ethanoic acid is used.
Pharmacodynamics
By suppressing enzyme , it disrupts the production of prostaglandins and ATP production. It has antipyretic and anti-inflammatory activity platelet aggregation .
The analgesic effect is due to both central and peripheral effects. In feverish conditions, it reduces the temperature by affecting the thermoregulation center.
Platelet aggregation and , as well as thrombus formation , are reduced due to the ability of ASA to suppress the synthesis of thromboxane A2 (TXA 2) in platelets. Inhibits the synthesis of prothrombin blood coagulation factor II ) in the liver and at a dose exceeding 6 g/day. — increases PTV.
Pharmacokinetics
Absorption of the substance after taking the drug orally is almost complete. The half-life of unchanged ASA is no more than 20 minutes. TCmax of ASA in blood plasma is 10-20 minutes, total salicylate formed as a result of metabolism is from 0.3 to 2.0 hours.
About 80% of acetylsalicylic and salicylic acids bound to albumin . Biological activity is maintained even when the substance is in protein-bound form.
Metabolized in the liver. Excreted by the kidneys. The pH of urine affects excretion: when it is acidified, it decreases, and when it is alkalized, it increases.
Pharmacokinetic parameters depend on the dose taken. Elimination of a substance is nonlinear. Moreover, in children of the 1st year of life, in comparison with adults, it proceeds much more slowly.
Acetylsalicylic acid
Registration number: P N003627/01
Trade name: Acetylsalicylic acid.
MNI or group name: Acetylsalicylic acid.
Dosage form: Tablets.
Composition per tablet: Active substance:
- Acetylsalicylic acid – 500 mg
Excipients:
- Potato starch - 91 mg
- Talc - 9 mg
Description: Tablets are white, slightly marbled, flat-cylindrical in shape with a chamfer and a score.
Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID).
ATX code: N02BA01
Pharmacological properties: The drug has an analgesic, antipyretic, and anti-inflammatory effect, which is due to the inhibition of cyclooxygenases involved in the synthesis of prostaglandins. Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane A2.
Pharmacokinetics: When taken orally, absorption is complete. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is quickly hydrolyzed by nonspecific plasma cholinesterases and albuminesterase, so the half-life is no more than 15-20 minutes. It circulates in the body (75 - 90% due to albumin) and is distributed in tissues in the form of salicylic acid anion. Time to reach maximum concentration is 2 hours. Serum concentration of salicylates is highly variable. Salicylates easily penetrate many tissues and body fluids, incl. into the cerebrospinal, peritoneal and synovial fluids. Penetration into the joint cavity accelerates in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. Salicylates are found in small quantities in nervous tissue, traces in bile, sweat, and feces. When acidosis occurs, most of the salicylic acid is converted into non-ionized acid, which penetrates well into tissues, incl. into the brain. It quickly passes through the placenta and is excreted in small quantities in breast milk. Metabolized primarily in the liver. Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. It is excreted primarily by active secretion in the renal tubules in the form of salicylic acid (60%) and in the form of metabolites. The excretion of salicylic acid depends on the pH of the urine (with alkalinization of the urine, the ionization of salicylates increases, their reabsorption worsens and excretion increases significantly). The rate of elimination depends on the dose: when taking small doses, the half-life is 2-3 hours, with increasing doses it can increase to 15-30 hours.
Indications for use: Treatment of moderate or mild pain: headache (including withdrawal symptoms), toothache, sore throat, back and muscle pain, joint pain, menstrual pain. Increased body temperature during colds and other infectious and inflammatory diseases (in adults and children over 15 years of age).
Contraindications:
- Hypersensitivity to acetylsalicylic acid and other NSAIDs or other components of the drug;
- Erosive and ulcerative lesions of the gastrointestinal tract (GIT) (in the acute phase);
- Gastrointestinal bleeding;
- Hemorrhagic diathesis;
- Concomitant use of methotrexate at a dose of 15 mg per week or more;
- Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid;
- Bronchial asthma induced by taking salicylates and other NSAIDs;
- Pregnancy (I and III trimester), breastfeeding period;
- Children's age (up to 15 years - when used as an antipyretic). The drug is not prescribed to children under 15 years of age with acute respiratory diseases caused by viral infections due to the risk of developing Reye's syndrome (encephalopathy and acute fatty liver with acute development of liver failure).
With caution: With concomitant therapy with anticoagulants, gout, gastric ulcer and/or duodenal ulcer (history), including chronic or recurrent peptic ulcer, or episodes of gastrointestinal bleeding; with renal and/or liver failure, glucose-6-phosphate dehydrogenase deficiency; hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergies, concomitant use of methotrexate at a dose of less than 15 mg/week, pregnancy (II trimester).
Use during pregnancy and lactation: During pregnancy, the use of the drug is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.
Method of administration and dosage: Orally, adults and children over 12 years of age: single dose is 250-500 mg, maximum single dose is 1.0 g (2 tablets of 500 mg), maximum daily dose is 3.0 g (6 tablets of 500 mg). mg), a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Children (as an analgesic) aged 6 to 12 years, with the exception of acute respiratory diseases caused by viral infections, due to the risk of developing Reye's syndrome (encephalopathy and acute fatty liver with acute development of liver failure), a single dose is 250 mg per dose, take up to 3 times a day.
Directions for use: The drug should be taken after meals with water, milk or alkaline mineral water.
Frequency and time of administration: A single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Regular adherence to the drug regimen allows you to avoid a sharp increase in temperature and reduce the intensity of pain. The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an analgesic and more than 3 days when prescribed as an antipyretic.
Side effects: From the gastrointestinal tract: Decreased appetite, abdominal pain, heartburn, nausea, vomiting, obvious (vomiting with blood, tarry stools) or hidden signs of gastrointestinal bleeding, which can lead to iron deficiency anemia, erosive - ulcerative lesions (including perforation) of the gastrointestinal tract, isolated cases of liver dysfunction (increased liver transaminases), diarrhea. From the central nervous system: Dizziness, tinnitus (usually signs of overdose); with long-term use - headache, blurred vision, decreased hearing acuity, aseptic meningitis. From the cardiovascular system: With long-term use - increased symptoms of chronic heart failure. From the hematopoietic system: Increased risk of bleeding, which is a consequence of the effect of acetylsalicylic acid on platelet aggregation, thrombocytopenia, anemia, leukopenia. From the excretory system: Impaired renal function; with long-term use - interstitial nephritis, prerenal azotemia with increased creatinine levels in the blood and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, edema. Allergic reactions: Skin rash, anaphylactic reactions, bronchospasm, Quincke's edema. Reye's syndrome (encephalopathy and acute fatty liver with rapid development of liver failure). If such symptoms appear, it is recommended to stop taking the drug and immediately consult your doctor.
Overdose: Symptoms: Moderate overdose: Nausea, vomiting, tinnitus, hearing loss, headache, dizziness and confusion. These symptoms disappear when the dose is reduced or the drug is discontinued. Severe overdose: Fever, hyperventilation, ketoacidosis, respiratory alkalosis, metabolic acidosis, coma, cardiogenic shock, respiratory failure, severe hypoglycemia. In chronic overdose, the concentration determined in plasma does not correlate well with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in elderly people when taking more than 100 mg/kg/day for several days. In children and elderly patients, the initial signs of salicylicism are not always noticeable, so it is advisable to periodically determine the concentration of salicylates in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - extremely severe, prognostically unfavorable. For moderate to severe poisoning, hospitalization is required.
Treatment: Hospitalization, gastric lavage, activated charcoal, monitoring of acid-base balance, alkalinization of urine in order to obtain a urine pH between 7.5 - 8 (forced alkaline diuresis is considered achieved if the concentration of salicylate in the blood plasma is no more than 500 mg /l (3.6 mmol/l) in adults or 300 mg/l (2.2 mmol/l) in children), hemodialysis, replacement of fluid loss, symptomatic therapy. Caution should be exercised in elderly patients in whom intensive fluid infusion may lead to pulmonary edema. The use of acetazolamide for alkalinization of urine is not recommended (it may cause acidosis and enhance the toxic effect of salicylates). Hemodialysis is indicated when the concentration of salicylates is more than 100 - 130 mg%, in patients with chronic poisoning - 40 mg% and lower if indicated (refractory acidosis, progressive deterioration, severe damage to the central nervous system, pulmonary edema and renal failure). For pulmonary edema, artificial ventilation of the lungs with an oxygen-enriched mixture.
Interaction with other drugs: Concomitant use:
- With methotrexate at a dose of 15 mg per week or more is a contraindication: the hemolytic cytotoxicity of methotrexate increases (renal clearance of methotrexate decreases and methotrexate is replaced by salicylates in connection with blood plasma proteins);
- With anticoagulants, for example, heparin: the risk of bleeding increases due to impaired platelet function, damage to the mucous membrane of the gastrointestinal tract, displacement of anticoagulants (indirect) from connection with blood plasma proteins;
- With other non-steroidal anti-inflammatory drugs: as a result of synergistic interaction, the risk of ulcers and bleeding from the stomach and duodenum increases;
- With uricosuric drugs, for example, benzbromarone: reduces the uricosuric effect;
- With digoxin: diogoxin concentration increases due to decreased renal excretion;
- With hypoglycemic drugs: the hypoglycemic effect of hypoglycemic drugs increases due to the hypoglycemic effect of acetylsalicylic acid;
- With drugs of the thrombolytic group: the fibrinolytic effect of the latter is enhanced and the risk of bleeding increases;
- With glucocorticosteroids, excluding hydrocortisone, used as replacement therapy for Addison's disease: when using glucocorticosteroids, the concentration of salicelates in the blood decreases due to increased excretion of the latter;
- With angiotensin-converting enzyme inhibitors: glomerular filtration is reduced due to inhibition of prostaglandin synthesis and, as a result, the antihypertensive effect is reduced;
- With valproic acid: the toxicity of valproic acid increases;
- With glucocorticosteroids, ethanol (alcoholic beverages) and ethanol-containing drugs: the risk of damaging the mucous membrane of the gastrointestinal tract increases, the risk of developing gastrointestinal bleeding increases;
- Enhances the effects of narcotic analgesics, indirect anticoagulants and antiplatelet agents, sulfonamides (including co-trimoxazole - increases their activity and toxicity), triiodothyronine (increases the activity and increases the risk of side effects of the latter);
- Reduces the effect of antihypertensive drugs, diuretics (spironolactone, furosemide);
- Increases the concentration of barbiturates and lithium salts in plasma;
- Antacids containing magnesium and/or aluminum slow down and impair the absorption of acetylsalicylic acid;
- Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Special instructions: Acetylsalicylic acid may cause bronchospasm, an attack of bronchial asthma or other hypersensitivity reactions. Risk factors are the presence of bronchial asthma, nasal polyps, fever, chronic bronchopulmonary diseases, and a history of allergies (allergic rhinitis, skin rashes). Acetylsalicylic acid may increase the tendency to bleeding, which is associated with its inhibitory effect on platelet aggregation. This should be taken into account when surgical interventions are necessary, including minor interventions such as tooth extraction. Before surgery, to reduce bleeding during surgery and in the postoperative period, you should stop taking the drug 5-7 days in advance and notify the doctor. Children should not be prescribed medications containing acetylsalicylic acid, since in the case of a viral infection the risk of Reye's syndrome increases. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, and liver enlargement. Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients. There was no effect of taking the drug on driving a vehicle and other mechanisms, which may affect the ability to drive vehicles, etc. Acetylsalicylic acid has a teratogenic effect; when used in the first trimester, it leads to the development of cleft palate; in the third trimester it causes inhibition of labor (inhibition of prostaglandin synthesis), premature closure of the ductus arteriosus in the fetus, pulmonary vascular hyperplasia and hypertension in the pulmonary circulation. It is excreted in breast milk, which increases the risk of bleeding in the baby due to impaired platelet function. During the treatment period, you should refrain from taking ethanol.
Release form: Tablets 500 mg. 10 tablets per blister-free or blister pack. One or two blister packs along with instructions for use are placed in a box made of cardboard. Contour cellless packages, together with an equal number of instructions for use, are placed in a group package.
Storage conditions: Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.
Shelf life: 4 years. Do not use the drug after the expiration date.
Conditions for dispensing from pharmacies: Without a prescription.
Indications for use: what do Acetylsalicylic acid tablets help with?
Indications for use of Acetylsalicylic acid are:
- febrile conditions in diseases of an infectious-inflammatory nature;
- rheumatoid arthritis;
- rheumatism;
- inflammatory damage to the myocardium , caused by an immunopathological reaction;
- pain syndrome of various origins, including headache and toothache (including headache associated with alcohol withdrawal syndrome), pain in joints and muscles, neuralgia, migraines , algodismenorrhea .
Also, aspirin (or acetylsalicylic acid) is used for prophylactic purposes in case of threat of thrombosis , thromboembolism , myocardial infarction (in case of myocardial infarction, the drug is prescribed for secondary prevention).
Indications and doses
Acetylsalicylic acid is prescribed for the following pathologies:
- febrile symptoms of inflammatory and infectious diseases;
- mild and moderate pain syndromes of various origins: migraine, neuralgic manifestations, myalgia;
- rheumatic joint damage;
- risk of thrombosis and thromboembolism;
- the risk of development and consequences of myocardial infarction;
- acute ischemic stroke;
- in complex therapy: alcohol withdrawal syndrome.
The recommended dose of the drug depends on the type and severity of the disease:
- for high fever, ARVI, pain - 100–500 mg three times a day;
- for intense fever - up to 1.5 g per day;
- for rheumatoid polyarthritis, other joint inflammations, myocardial diseases - up to 4 g daily.
Acetylsalicylic acid should be taken after meals. It is recommended to grind the non-coated tablets into powder and wash them down with plenty of warm water. You can use a slightly alkaline mineral one. The effervescent drug must first be dissolved in 50–60 ml of liquid. In liquid form, acetylsalicylic acid is absorbed faster into the blood and has less contact with the gastric mucosa.
Contraindications
Taking ASA is contraindicated in:
- “aspirin” asthma;
- during the period of exacerbation of erosive and ulcerative lesions of the digestive canal ;
- stomach/intestinal bleeding;
- vitamin deficiency K;
- hemophilia , hypoprothrombinemia , hemorrhagic diathesis ;
- G6PD enzyme deficiency
- portal hypertension;
- renal/liver failure;
- aortic dissection;
- during treatment with Methotrexate (if the weekly dose of the drug exceeds 15/mg);
- gouty arthritis, gout;
- pregnancy (absolute contraindications are the first three and last three months);
- breastfeeding;
- hypersensitivity to ASA/salicylates.
Side effects
Side effects of ASA treatment may include:
- nausea;
- gastralgia;
- anorexia;
- allergic reactions;
- diarrhea;
- thrombocytopenia;
- erosive and ulcerative lesions of the digestive canal;
- renal and/or liver failure.
With prolonged use, tinnitus appears, hearing acuity decreases, vision is impaired, dizziness occurs and, when taking high doses, headaches. Bleeding, hypocoagulation , vomiting, and bronchospasm .
Acetylsalicylic acid, instructions for use (Method and dosage)
For active rheumatism, adult patients are prescribed 5 to 8 g of ASA per day. For a child, the dose is calculated depending on weight. As a rule, it varies from 100 to 125 mg/kg/day. Frequency of use: 4-5 rubles/day.
1-2 weeks after the start of the course, the dose for a child is reduced to 60-70 mg/kg/day; for adult patients, the dosage remains the same. Treatment should be continued for up to 6 weeks.
According to the instructions for use of Acetylsalicylic acid, the drug should be discontinued gradually over 1-2 weeks.
Acetylsalicylic acid for headaches and as a remedy for fever is prescribed in lower dosages. Thus, for pain and feverish conditions, the dose per 1 dose for an adult is from 0.25 to 1 g with a frequency of use from 4 to 6 times per day.
It should be remembered that for headaches, ASA is especially effective if the pain is provoked by an increase in ICP (intracranial pressure).
For children, the optimal dose per dose is 10-15 mg/kg. Frequency of applications - 5 rubles/day.
Treatment should not last more than 2 weeks.
To prevent thrombosis and embolism, ASA is taken 2-3 times a day. 0.5 g each. To improve the rheological properties (to thin the blood the drug is taken for a long time at 0.15-0.25 g/day.
For a child over five years of age, a single dosage is 0.25 g, four-year-old children are allowed to be given a single dose of 0.2 g of ASA, two-year-old children - 0.1 g, one-year-old children - 0.05 g.
It is forbidden to give ASA to children for fever that rises due to a viral infection . The drug acts on the same structures of the brain and liver as some viruses, and in combination with a viral infection can provoke the development of Reye's syndrome .
Application of ASA in cosmetology
A face mask with Acetylsalicylic acid allows you to quickly relieve inflammation, reduce tissue swelling, remove redness, remove the surface layer of dead cells and clean clogged pores.
The drug dries the skin well and is perfectly soluble in fats, which makes it advisable to use it as a remedy for acne : tablets, moistened with water, are applied to inflamed elements on the face or added to face masks.
Acetylsalicylic acid for acne works well in combination with lemon juice or honey. A clay mask is also effective for eliminating skin problems.
To prepare a lemon-aspirin mask, tablets (6 pieces) are simply ground with freshly squeezed juice until smooth. Then the medicine is applied pointwise to the inflamed pimples and left on them until they dry.
A mask with honey is prepared as follows: tablets (3 pieces) are moistened with water, and then, when they dissolve, mixed with 0.5-1 teaspoon (teaspoon) of honey.
To prepare a clay mask, mix 6 crushed ASA tablets and 2 teaspoons of white/blue clay with warm water.
Composition and effectiveness
In its pure form, ASA is a white, finely crystalline powder with a noticeably sour taste. It is an acetic ester, soluble in water and alcohols. The drug quickly relieves pain and has a pronounced antipyretic, anti-inflammatory, and antiplatelet effect. Its effectiveness is similar to other NSAIDs - non-narcotic analgesics.
- The analgesic properties of ASA are due to its effect on the central nervous system, the activity of prostaglandins and other mediators of pain sensitivity.
- A decrease in body temperature occurs due to the correction of the thermoregulation center, vasodilation and a pronounced diaphoretic effect.
- Inflammatory reactions are eliminated due to the effect of acetylsalicylic acid on the capillary network: reducing the permeability of vascular walls, blocking enzymatic and energetic activity in pathological foci.
- Aspirin has the ability of an anticoagulant: it prevents platelet aggregation (sticking together), slows down the synthesis of prothrombin, which is responsible for blood clotting. This reduces the risk of thrombosis and associated life-threatening conditions.
Acetylsalicylic acid is absorbed almost completely into the bloodstream from the stomach cavity within 10–15 minutes. Severe symptoms of the disease subside immediately:
- dizziness, headache, joint and muscle pain decreases;
- temperature indicators decrease;
- the feeling of heat and other signs of malaise disappear.
As a result of taking aspirin, a decrease in temperature in patients is often accompanied by profuse sweating.
The decay period of acetylsalicylic acid in the body is about 1–2 hours. Metabolites are excreted in the urine. The therapeutic effect of the drug persists for some time.
Due to its rapid therapeutic effect and effectiveness in treating a variety of diseases, acetylsalicylic acid is classified as an emergency medicine and is on the list of vital drugs.
Overdose
Overdose can result from:
- long-term treatment with ASA;
- single administration of too high a dose of the drug.
A sign of overdose is salicylic syndrome , manifested by general malaise, hyperthermia, tinnitus, nausea, and vomiting.
Severe intoxication is accompanied by convulsions , stupor, coma , severe dehydration, non-cardiogenic pulmonary edema , renal failure , impairment of CBS, shock.
In case of an overdose of ASA, the victim should be immediately hospitalized. His stomach is washed, he is given activated carbon , and his CBS is checked.
Depending on the condition of the CBS and the balance of water and electrolytes, the administration of solutions of sodium lactate , sodium citrate and sodium bicarbonate (in the form of infusion) may be prescribed.
with alkaline diuretics is required .
In case of severe intoxication, hemodialysis ; replenish fluid loss; symptomatic treatment is prescribed.
Interaction
Increases the toxicity of barbituric drugs , valproic acid , methotrexate , the effects of oral hypoglycemic drugs, Digoxin , narcotic analgesics , Triiodothyronine , sulfonamide drugs .
Weakens the effects of diuretics (potassium-sparing and loop), antihypertensive drugs from the group of ACE inhibitors, and the effect of uricosuric drugs .
When used simultaneously with antithrombotic drugs , thrombolytics , indirect anticoagulants, it increases the risk of bleeding.
GCS enhance the toxic effect of ASA on the mucous membrane of the digestive canal, increase its clearance and reduce plasma concentration.
When used simultaneously with Li salts, it increases the plasma concentration of Li+ ions.
Strengthens the toxic effect of alcohol on the mucous membrane of the digestive canal.
Description of the drug ACETYLSALICYLIC ACID
When used simultaneously, antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.
With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.
When used simultaneously with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents, sulfonylurea derivatives, insulins, methotrexate, phenytoin, and valproic acid is enhanced.
When used simultaneously with GCS, the risk of ulcerogenic effects and gastrointestinal bleeding increases.
With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.
With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid may reduce plasma concentrations of indomethacin and piroxicam.
When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.
With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) is reduced.
With the simultaneous use of acetylsalicylic acid and sodium alendronate, severe esophagitis may develop.
With simultaneous use of griseofulvin, the absorption of acetylsalicylic acid may be impaired.
A case of spontaneous hemorrhage into the iris was described when taking Ginkgo biloba extract during long-term use of acetylsalicylic acid at a dose of 325 mg/day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.
With simultaneous use of dipyridamole, an increase in Cmax of salicylate in blood plasma and AUC is possible.
When used simultaneously with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.
With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible.
Acetylsalicylic acid in doses less than 300 mg/day has a minor effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, the effectiveness of captopril and enalapril may be reduced.
With simultaneous use, caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.
With simultaneous use, metoprolol may increase the Cmax of salicylate in the blood plasma.
When using pentazocine against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing severe adverse reactions from the kidneys.
With simultaneous use, phenylbutazone reduces uricosuria caused by acetylsalicylic acid.
With simultaneous use, ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.
special instructions
The drug should be used with caution in people with pathologies of the kidneys and liver , bronchial asthma , with increased bleeding, decompensated CHF, during treatment with anticoagulants, as well as in people with a history of erosive and ulcerative lesions of the digestive tract and/or gastric/intestinal bleeding .
Even in small doses, ASA reduces the excretion of uric acid , which can cause an acute attack of gout .
When taking high doses of ASA or needing long-term treatment with the drug, it is necessary to regularly monitor hemoglobin and see a doctor.
As an anti-inflammatory agent, use ASA at a dose of 5-8 g/day. limited due to the increased risk of adverse reactions from the gastrointestinal tract.
To reduce bleeding during surgery and in the postoperative period, salicylates should be stopped 5-7 days before surgery.
When taking ASA, you should remember that this drug can be taken for pain relief for no more than 7 days without consulting a doctor. As an antipyretic, ASA is allowed to be taken for no more than 3 days.
Chemical properties of the substance
When ASA crystallizes, colorless needles or monoclinic polyhedra with a slightly sour taste are formed. The crystals are stable in dry air, but with increasing humidity they gradually hydrolyze to salicylic and acetic acids.
The substance in its pure form is a white crystalline powder and practically odorless. The appearance of an acetic acid odor is evidence that the substance has begun to hydrolyze.
ASA undergoes esterification under the influence of alkaline bicarbonates, alkaline hydroxides, and also in boiling water.
ASA is poorly soluble in water, soluble in chloroform and ether, and easily soluble in 96% ethanol. The solubility of ASA in water/aqueous media is strongly influenced by the pH level: the higher the alkalinity of the solvent, the more easily the substance dissolves.
Description of the drug ASPIRIN
When used simultaneously, antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.
With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.
When used simultaneously with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents, sulfonylurea derivatives, insulins, methotrexate, phenytoin, and valproic acid is enhanced.
When used simultaneously with GCS, the risk of ulcerogenic effects and gastrointestinal bleeding increases.
With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.
With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid may reduce plasma concentrations of indomethacin and piroxicam.
When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.
With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) is reduced.
With the simultaneous use of acetylsalicylic acid and sodium alendronate, severe esophagitis may develop.
With simultaneous use of griseofulvin, the absorption of acetylsalicylic acid may be impaired.
A case of spontaneous hemorrhage into the iris was described when taking Ginkgo biloba extract during long-term use of acetylsalicylic acid at a dose of 325 mg/day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.
With simultaneous use of dipyridamole, an increase in Cmax of salicylate in blood plasma and AUC is possible.
When used simultaneously with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.
With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible.
Acetylsalicylic acid in doses less than 300 mg/day has a minor effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, the effectiveness of captopril and enalapril may be reduced.
With simultaneous use, caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.
With simultaneous use, metoprolol may increase the Cmax of salicylate in the blood plasma.
When using pentazocine against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing severe adverse reactions from the kidneys.
With simultaneous use, phenylbutazone reduces uricosuria caused by acetylsalicylic acid.
With simultaneous use, ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.
Analogs
Level 4 ATC code matches:
Aspirin-S
Citropak
Aspirin
Citramon
Coficil-Plus
Farmadol
Askofen-P
Cefekon N
Aquacitramon
Upsarin UPSA
Citrapack
Alca Prim
Thrombopol
Citrapar
Acetylsalicylic acid-UBF, Asprovit , Aspinat , Aspivatrin , Nextrim Fast , Fluspirin , Taspir , Aspirin.
For children
In children, ASA cannot be used for hyperthermia associated with a viral infection , since this combination can cause the development of a life-threatening condition for the child - Reye's syndrome .
In newborn infants, salicylic acid can displace bilirubin from its association with albumin and contribute to the development of encephalopathy .
ASA easily penetrates into all fluids and tissues of the body, including cerebrospinal, synovial and peritoneal fluid.
In the presence of edema and inflammation, the penetration of salicylate into the joint cavity is accelerated. In the stage of inflammation, on the contrary, it slows down.
Acetylsalicylic acid and alcohol
Alcohol during the period of ASA is contraindicated. This combination can cause gastric and intestinal bleeding, as well as severe hypersensitivity reactions.
What is Acetylsalicylic acid used for hangovers?
ASA is a very effective hangover remedy, due to the antiplatelet effect of the drug.
However, you should remember that it is better to take the tablet not while drinking alcohol, but about 2 hours before the feast. This reduces the risk of microthrombi in small vessels of the brain and, partly, tissue edema.
Acetylsalicylic acid, 500 mg, tablets, 10 pcs.
When used simultaneously, antacids containing magnesium and/or aluminum hydroxide slow down and reduce the absorption of acetylsalicylic acid.
With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.
When used simultaneously with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents, sulfonylurea derivatives, insulins, methotrexate, phenytoin, and valproic acid is enhanced.
When used simultaneously with GCS, the risk of ulcerogenic effects and gastrointestinal bleeding increases.
With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.
With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid may reduce plasma concentrations of indomethacin and piroxicam.
When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.
With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) is reduced.
With the simultaneous use of acetylsalicylic acid and sodium alendronate, severe esophagitis may develop.
With simultaneous use of griseofulvin, the absorption of acetylsalicylic acid may be impaired.
A case of spontaneous hemorrhage into the iris was described when taking Ginkgo biloba extract during long-term use of acetylsalicylic acid at a dose of 325 mg/day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.
With simultaneous use of dipyridamole, an increase in salicylate C max in blood plasma and AUC is possible.
When used simultaneously with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.
With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible.
Acetylsalicylic acid in doses less than 300 mg/day has a minor effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, the effectiveness of captopril and enalapril may be reduced.
With simultaneous use, caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.
With simultaneous use, metoprolol may increase the Cmax of salicylate in the blood plasma.
When using pentazocine against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing severe adverse reactions from the kidneys.
With simultaneous use, phenylbutazone reduces uricosuria caused by acetylsalicylic acid.
With simultaneous use, ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.
Use during pregnancy and breastfeeding
Acetylsalicylic acid is contraindicated during pregnancy. Especially in the first and last three months of gestation. In the early stages, taking the drug can increase the risk of developing birth defects; in the later stages, it can lead to post-term pregnancy and weakening of labor.
ASA and its metabolites pass into milk in small quantities. After accidentally taking the drug, no side effects were observed in infants, and therefore, interrupting breastfeeding (BF) is usually not necessary.
If a woman is indicated for long-term treatment with high doses of ASA, it is necessary to stop breastfeeding.
Can pregnant women take acetylsalicylic acid?
Pregnancy and breastfeeding are contraindications for the use of aspirin. This is especially true for the 1st and 3rd trimesters. Using the medicine in the early stages can increase the risk of birth defects, and taking it in recent months can lead to post-term pregnancy.
The active substance can pass into breast milk in small quantities. When children accidentally took the drug, no adverse reactions appeared, but it is still worth refraining from taking it. If a woman is prescribed long-term use of aspirin, then breastfeeding must be interrupted for the entire course of treatment.
Reviews
Almost all reviews left about ASK are positive. The drug is inexpensive, effective, well studied, and has a wide range of applications. The tablets perfectly relieve inflammation and fever, and regular use of ASA in small doses can reduce the risk of cardiovascular complications in predisposed patients.
Potential side effects are usually referred to as the disadvantages of the drug. However, as most people note, to avoid them, during the treatment period it is enough to simply follow certain rules: at a minimum, before taking the pills, you should carefully read the instructions and give up alcohol for the entire treatment period.
Acetylsalicylic acid price
The price of ASK in Ukraine is from 2.88 UAH, in Russia - from 7 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Acetylsalicylic acid tablets 500 mg 20 pcs. Pharmstandard-Leksredstva OJSC
21 rub. order - Acetylsalicylic acid Medisorb tab. 0.5g 30pcs JSC Medisorb
33 rub. order
- Acetylsalicylic acid Renewal tab. p/o captivity. 500 mg 20 pcs JSC "PFK Obnovlenye"
94 RUR order
- Acetylsalicylic acid Cardio tab. intestinal p/o captivity. 0.05g 30pcs JSC Alium
57 RUR order
- Acetylsalicylic acid cardio tab. p.o ksh/sol. 100mg 30pcs JSC Obolenskoe farm. company
67 RUR order
Pharmacy Dialogue
- Acetylsalicylic acid Renewal (tab.p.pl/vol. 500 mg No. 20)Update of PFC CJSC
77 RUR order
- Acetylsalicylic acid Renewal (tab.p.pl/vol. 500 mg No. 20)Update of PFC CJSC
78 RUR order
- Acetylsalicylic acid tablets 500 mg No. 10FS.-Leksredstva
8 rubles order
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Pharmacy24
- Acetylsalicylic acid (Aspirin) 500 mg No. 10 tablets PAT "Kiivmedpreparat", Ukraine/PAT "Galichfarm", Ukraine
7 UAH. order - Acetylsalicylic acid (Aspirin) 500 mg No. 10 tablets PAT "Lubnipharm", Ukraine
3 UAH order
- Acetylsalicylic acid (Aspirin) 500 mg No. 10 tablets PAT Monfarm, Ukraine
3 UAH order
- Acetylsalicylic acid Darnitsa (Aspirin) No. 10 tablets PrAT" Pharmaceutical company "Darnitsa", Ukraine
6 UAH order
PaniPharmacy
- Acetylsalicylic acid tablets Acetylsalicylic acid tablets. 0.5g No. 10 Ukraine, Monfarm JSC
3 UAH order
- Acetylsalicylic acid tablets Acetylsalicylic acid tablets. 0.5g No. 10 Ukraine, Lubnyfarm PJSC
3 UAH order
- Acetylsalicylic acid tablets Acetylsalicylic acid tablets. 0.5g No. 10 Ukraine, Kievmedpreparat OJSC
7 UAH order
- Acetylsalicylic acid tablets Acetylsalicylic acid tablets. 0.05g No. 10 Ukraine, Tekhnolog ChAO
3 UAH order
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